NR 566 Week 6 Study Guide Chapter 22: Drugs Affecting the Reproductive System

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NR 566 Week 6 Study Guide Chapter 22: Drugs Affecting the Reproductive System • Know the pharmacodynamics, pharmacotherapeutics, clinical use, drug interactions, and ADRs for: Erectile dysfunctio... n (ED) drugs, Estrogens and Progesterone, and Antiandrogen drugs • Androgen drugs o Testosterone is the primary male androgen o Responsible for: ▪ Growth, maturation, and maintenance of male sex organs and secondary sexual characteristics ▪ Skeletal growth spurt in adolescence and termination of linear growth by fusion of the epiphyseal growth plate ▪ Activation of sebaceous glands (acne during puberty) ▪ Enhances production of erythropoietic stimulating factor, increased RBCs production ▪ Libido o Androgen Drugs: testosterone propionate (in oil, DepoTesterone), testosterone enanthate (in oil, Delatestryl), testosterone cypionate (in oil, Depo-Testosterone), methyltestosterone (Android, Methitest, Testred, Virilon), testosterone gel (AndroGel 1%, AndroGel 1.62%, Axiron, Testium), fluoxymesterone, TD testosterone (Testoderm, Androderm), and buccal testosterone (Striant) ▪ Used to treat Indicated for the symptomatic Tx of • 1) deficiency states in males associated with hypogonadism and • 2) in both sexes for d/os such as CA and HIB, Tx libido, endometriosis, and postmenopausal symptoms in women, have been used illicitly to enhance athletic performance and increase muscle mass o Contraindicated: male breast CA, prostate CA, and Pregnancy (Category X), and lactation • Antiandrogens: several different categories o Androgen hormone inhibitors (5-alpha-reductase inhibitors) ▪ Drugs: Finasteride (Propecia, Proscar) and dutasteride (Avodart) ▪ MOA: Block conversation of testosterone to dihydrotesterone ▪ Used to Tx BPH ▪ PSA levels and digital prostate examination are required monitoring for men on these agents ▪ Finasteride (Propecia, Proscar): • Extensive hepatic metabolism • BPH: 5mg/day, 6 to 12 months of therapy until therapeutic response o Regression of prostate size increased urinary flow, and improve BPH symptoms • Approved for Male pattern baldness: 1 mg/day, three months until results • Stopping the drugs reverses the effect within 12 months • ADRs: decreased libido, impotence (can occur at both doses) ▪ Dutasteride (Avodart) • Inhibits both type 1 and 2 (5-alpha-reductase) • Peak clinical effect 6 to 12 months of therapy • Extensively metabolized in the liver (CYP3A4 and CYP3A5) • Used to Tx BPH • Absorbed through the skin, women who are pregnant or may become pregnant should not handle dutasteride capsules r/t risk of fetal anomaly to a male fetus • ADR: decreased libido and impotence o Gonadotropin-releasing hormone analogue: luteinizing hormone-releasing hormone antagonist ▪ Leuprolide acetate (Lupron) ▪ Create a reversible chemical orchiectomy state in males and an oophorectomy state in females ▪ Used to Tx: advanced prostatic CA and for management of endometriosis and uterine leiomyomata (fibroids) ▪ 1 mg SC daily or IM every 3 months (depot formulation) ▪ Increased suppression when used with flutamide (direct antiandrogen) ▪ Peds: Tx central precocious puberty ▪ Women: reducing uterine fibroids, endometriosis, and PCOS (pain relief, regain fertility) o Direct antiandrogens ▪ Flutamide (Eulexin), bicalutamide (Casodex), and nilutamide (Nilandron) ▪ Inhibit androgen uptake or nuclear binding of androgen at target tissues ▪ Uses as part of combo therapy Tx of prostatic carcinoma ▪ Flutamide: competitive antagonist at the androgen receptor site • Truly a nonsteroidal agent • ADRs: gynecomastia and reversible liver toxicity • Renal doses: less than 29 mL/min • BLACK BOX WARNING: hepatic failure, hepatic encephalopathy, and death o Usually within the first 3 months of therapy o Baseline and monthly LFTs for the first 4 months of therapy and periodically o D/c if any symptoms of hepatic injury or jaundice develop o Spironolactone (Aldactone): aldosterone antagonist and inhibitor of 5-alpha-reductase ▪ used as a K sparing diuretic ▪ Off label use for Tx of female hirsutism and acne due to antiandrogenic properties • 50 to 200 mg/day ▪ Competitive inhibitor of the dihydrotestosterone, aldosterone, and interferes with the androgen receptors in the prostate • Also reduces 17-alpha-hydroxylase activity: lowers plasma levels of testosterone and androstenedione ▪ Metabolized by the liver ▪ Short term use for primary hyperaldosteronism in patients preoperatively ▪ Long term: for those who are not good candidates for Sx with idiopathic hyperaldosteronism ▪ PMS/PMDD symptoms may be relieved by spironolactone (25 mg QID beginning on day 14 of the menstrual cycle) ▪ ADRs: dose-related and reversible when the drug is d/c GI upset, drowsiness, gynecomastia, impotence, cutaneous eruptions, and urticaria ▪ BLACK Box Warning: r/t animal chronic toxicity studies demonstrated tumorigenicity ▪ Contraindications: pregnancy • Drug Interactions o Finasteride: Nevirapine: Combo induces hepatic metabolism of finasteride: monitor f [Show More]

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